Anti-cellulite liposomal agent

FIELD: cosmetology.

SUBSTANCE: invention is anti-cellulite liposomal agent comprising enclosed in liposomes of lecithin water-soluble extracts of southern sumac (Buxus sinica) and anise (Pimpinella anisum), enclosed in the inner phase of liposomes, and oil-soluble extract of pink pepper (Schinus terebinthifolius) enclosed in an outer casing of liposomes.

EFFECT: natural and induced lipolysis and inhibition of lipogenesis process after meal.

4 cl, 3 ex, 1 tbl, 2 dwg

 

The invention relates to pharmacology and cosmetology, and in particular to means for skin care, and primarily aimed at the elimination of edema, improving tone and elasticity of the skin, normalization of lipid metabolism, and mainly, to prevent and eliminate cellulite.

Despite the large number of different tools to combat cellulite, what causes it remain unexplored. Important in the pathogenesis of cellulite assign heredity, immobility, metabolic and hormonal disorders.

Cellulite is a local increase of fat cells (adipocytes) and the circulation in adipose tissue. Adipocytes cease to highlight the products of their metabolism, but with a vengeance accumulate fats (lipids).

The transformation of fats and their introduction into the circulatory system occurs due to adipocytes. For normal skin is characterized by the presence of adipocytes small size. The pathological process of cellulite is stagnant lymph and interstitial fluid, which increases its viscosity and ultimately rebirth in fibrous tissue is the formation of so-called nodules, which felt good on the skin at the extreme cellulite (orange skin). The reason for these changes is the violation of the functions of adipocytes, which have accumulated lipids.

In subcutaneous adipose tissue adipocytes are located in the thickness of the elastic and connective tissue fibers. In different pathologies, including human nutrition, adipocytes can become more than you need, they increase in size. All this leads to compression of the blood and lymph vessels that disrupts the natural fluid flow to the tissues worse receives nutrients and oxygen from the tissues toxins. Intercellular fluid stagnates.

Nowadays, there are many methods for cellulite reduction, the action of which is directed at maintaining the normal state of the skin and to prevent cellulite to develop. The basic principles of the fight against cellulite are the improvement of blood circulation in the subcutaneous fat and the elimination of harmful factors. It uses a variety of cosmetic products at home and in beauty salons, where professionals come to the aid of special devices.

It is known that many cosmetic products are more effective when used in liposomal form.

Liposomes are microscopic closed vesicles having an internal phase, surrounded by one or more lipid bilayers, and ability to hold water-soluble mA is Arial in the internal phase, and oil-soluble material in Phospholipides bilayer. At the conclusion of the active substance in the liposome and its delivery to the target tissue important tasks are highly efficient capture of the active compound in the liposome and sustainable retention of the active compounds of the liposome. Liposomes can be made of phospholipids, particularly phosphatidylcholine, phosphatidylethanolamine, phosphatidylserine, phosphatidylinositol, phosphatidylglycerol, fosfatados acid, sphingophospholipids, phospholipids, egg or soy beans, or mixtures thereof.

In General, it is believed that the liposome is a particle with a predominant size from a few tens of nanometers up to several tenths of microns, inside the shell of which is composed of phospholipid, which are molecules of the other substance (s). The membrane of liposomes is semi-permeable to water molecules and ions.

For liposomes characterized by the ability to include and retain substances of different nature. The range of substances included in liposomes, is quite wide - from inorganic ions and low molecular weight organic compounds to large proteins and nucleic acids.

Liposomes interact with cells as ordinary particles obeying the laws of diffusion particles. In particular, they are in contact with cells with a high degree of adhesion is Known, what liposomes easily penetrate through the outer cell membrane, and easily contact membrane structures up to embed in their patterns.

Liposomes have several advantages: able to strengthen the skin's barrier function, have structural similarity with biological membranes in the body that can include both water - and oil-soluble components, have high bioavailability, etc.

Liposomes can easily interact with the membranes of living cells and provide a rapid elimination of the deficit phospholipids.

Liposomes provide a prolonged release of a prisoner in a carrier substance.

The ability of liposomal particles to deform the structure in the process of overcoming the microcapillaries Horny and brilliant layers of the epidermis is another feature of liposomes.

Using the conclusion in liposomes not only to deliver biologically active substances to the desired skin depth, exactly to the goal, but in many cases significantly reduce their required concentration, thereby reducing the risk of allergic or sensitizing reactions.

Methods to form liposomes are diverse and can be divided into three main groups:

- thin-film methods;

- methods based on the use of solvents;/p>

- ultrasonic method;

methods using high pressure.

The beauty industry today offers numerous anti-cellulite preparations in a variety of forms: gels, lotions, scrubs, creams, essential oils, etc. They are simple, easy to use and hygienic. In the early stages of such funds may suspend the distribution process cellulite.

Scrubs and peels remove dead skin cells, promote tissue oxygenation, resulting in increased tone.

Anti-cellulite creams provide drainage of fluid from the fat tissues through the lymphatic system and improve skin tone.

Well-known cosmetic composition for combating cellulite, which includes the active ingredients from the group consisting of collagen, eurocasino, elastin, amino acids, peptides, mucopolysaccharides, or from the group consisting of vitamins, hormones, antibiotics (EN 2126243).

The disadvantage of this tool is that the active ingredients listed below, in addition to the hormones of any appreciable anti-cellulite effect on the problem areas do not have; the use of hormones, as a rule, it is undesirable or even unacceptable in cosmetic preparations because of the harmful side effects.

Known cosmetic composition having anti-cellulite properties is AMI, which includes herbal ingredients, including essential oil of rosemary (US 4795638).

Known composition has basically just vasomotor, toning effect; its use is very difficult, as connected with the necessity of thermocautery, which are produced mainly in special cosmetic treatments.

Known cosmetic product with anti-cellulite effect, including essential oils of grapefruit and rosemary, as well as several other herbal ingredients (patent DE 19718848).

The disadvantage of it is that it provides stimulation of blood and lymph flow, mainly in the place of its application, and to some very small degree stimulates lipolysis and fat breakdown.

In addition, almost all manufacturers of anti-cellulite preparations combine the cream with other procedures to enhance its effect. The cream is best to RUB into the skin after exercise or active self-massage, peeling, shower.

The technical task of the present invention is the creation of the anti-money effectively "working" under any circumstances: at rest, during exercise and stress, after a meal, and helps to slow down the formation of adipocytes (fat cleto is). This leads to a significant reduction of fat deposition in adipose tissue, to improve the appearance and properties of the skin, eliminate "orange peel".

To solve this problem proposed liposomal anti-cellulite agent, characterized in that it includes a enclosed in the liposomes of lecithin water-soluble extracts of Smoke tree (Buxus sinica) and Anise (Pimpinella anisum) and oil-soluble extract of Pink pepper (Schinus terebinthifolius), with water-soluble extracts of Smoke tree (Buxus sinica) and Anise (Pimpinella anisum) is enclosed in the internal phase of the liposome, and oil-soluble extract of Pink pepper (Schinus terebinthifolius) is enclosed in the membrane of liposomes.

It is preferable that the content of lecithin in the medium is from 5 to 25 wt.%.

It is preferable that, as the use of lecithin soy lecithin.

Preferably, that means the content of the oil-soluble extract of Pink pepper is from 0.1 to 1 wt.%, the content of water-soluble extract of Cotinus is from 1 to 10 wt.%, and the content of water-soluble extract of Anise from 1 to 10 wt.%.

In necessary cases, according to the recipe and practical application of cosmetics offered liposomal tool may contain the necessary cosmetic additives such as an antioxidant and preservative, with the following content, wt.%:

Lecithinfrom 5 to 25
Extract of Pink pepperfrom 0.1 to 1
Extract of Cotinusfrom 1 to 10
Anise extractfrom 1 to 10
Antioxidantfrom 0.01 to 3
Preservativefrom 0.5 to 2
Waterrest

While it is preferable to use as an antioxidant equivalent and/or Tocopherols, and as preservatives - parabens, and/or diazolidinyl urea, and/or imidazolidinyl urea, commonly used in cosmetic products.

The proposed anti-cellulite liposomal tool allows you to:

Due to the water-soluble extracts of smoke and anise:

- to carry out natural lipolysis (the breakdown of fats into its constituent fatty acids under the action of the enzyme lipase) due to activation cleavage of triglycerides in the quiescent state;

- to exercise-induced lipolysis, i.e. to accelerate the breakdown of fats during exercise and stress;

to inhibit the process of lipogenesis, i.e. execute the inhibition of the formation of triglycerides after a meal;

Due to the oil-soluble extract of Pink pepper is the inhibition of the formation of large adipocytes and fat accumulation, because the extract reduces protein synthesis Perilipin that protects body cells from the action of the enzyme lipase.

The combined effect of extracts allows adipokines, i.e. to slow down the formation of adipocytes.

As shown by the study authors, the most effective joint action of extracts appears at the conclusion in liposomal form: water-soluble extracts of smoke and anise are enclosed in the inner cavity of liposomes and oil-soluble extract of pink pepper is included in the membrane of liposomes. This allows you to deliver biologically active substances to the desired skin depth.

Plant extracts can be obtained by traditional methods of extraction, such as water-alcohol and oil extraction ("Chemistry and technology of herbal remedies" S.A. Minin and IE Kauhava. Textbook for high schools. Moscow, 2004), but it is preferable to obtain extracts of smoke and anise method cryoextraction ((Generals could BE the Main cryochemical processes nanotechnology: Theory and methods of calculation: the textbook for high schools. - St. Petersburg: " "Profession", 2010. - 349 S.), and pink pepper extract is from the seeds of Schinus terebinthifolius using supercritical CO2 is straccia. (http://www.extract.ru/index.php?id=94).

To obtain the proposed anti-cellulite liposomal means first prepare prizemoney.

A mixture of 1)

Mix between a calculated amount of water (t=30-45C), extract of cotinus (at a concentration of 1.0-10.0 wt.%), the anise extract (concentration of 1.0-10.0 wt.% and lecithin (at a concentration of 5.0 to 25.0 wt.%) and continue mixing until a homogeneous mass.

Mix 2)

As between themselves when heated to 45C mix the pink pepper extract (at a concentration of 0.1-1.0 wt.%) and antioxidant (at a concentration of 0.01 to 3 wt.%) and continue stirring until a homogeneous liquid.

Then in a mixture of 1) add mixture 2) and preservative (in a concentration of 0.5-2.0 wt%) and intensively mixed in ultrameal (speed up to 15,000 rpm). Predementia ready.

Then prepare liposomes.

The resulting prizemoney homogenized in the homogenizer high pressure (2 cycle) at an operating pressure varying between 250 and 600 bar.

As an antioxidant can be used equivalent, Tocopherols, and mixtures thereof. As preservative can be used in a variety of parabens, diazolidinyl urea, imidazolidinyl urea, and mixtures thereof.

The following examples illustrate various options for cosmetic products with a description of the retrieval method that is not limited the invention in essence.

Example 1. Anti-cellulite liposomal agent.

In water (up to 100 kg) temperature 30C add 6 kg of the extract smoke, 6 m extract of anise, 16 kg of lecithin and mix all until smooth. Next, we take 0.6 kg of the extract of pink pepper, add to it 0,06 kg of antioxidant of butylhydroxytoluene, heated with stirring to 45C and continue to stir until complete dissolution of butylhydroxytoluene. Then 1 kg of preservative, Germaben and the mixture butylhydroxytoluene blended with pink pepper added to a mixture of water, lecithin, extracts of smoke and anise. Next, using high-speed stirrers Ultra Turrax for 10 min with a speed of 1500 Rev/min through an intensive mixing of the mass. The resulting mixture is expanded through a high-pressure homogenizer. Spend 2 cycle run, the working pressure is 600 ATM.

The resulting tool is a time-stable liposomes with high efficiency to the inclusion of active substances. Stability of liposomes is confirmed by a test for accelerated aging and study them under a microscope. Time also does not change the appearance of liposomal products (differentiation, heterogeneity, and so on). The resulting tool has anti-cellulite properties, reparative action, the us is ranaut swelling, improves the tone and elasticity of the skin, normalizes lipid metabolism.

Example 2. Anti-cellulite liposomal agent.

In water (up to 100 kg) temperature 30C add 6 kg of the extract of cotinus, 6 kg of the extract of anise, 2 kg of lecithin and mix all until smooth. Next, we take 0.6 kg of the extract of pink pepper, add to it 0,06 kg of antioxidant butylhydroxytoluene, heated with stirring to 45C and continue to stir until complete dissolution of butylhydroxytoluene. Then 1 kg of preservative, Germaben and the mixture butylhydroxytoluene blended with pink pepper added to a mixture of water, lecithin, extracts of smoke and anise. Next, using high-speed stirrers Ultra Turrax for 10 min with a speed of 1500 Rev/min conducting intensive mixing of the mass. The resulting mixture is expanded through a high-pressure homogenizer. Spend 2 cycle run, the working pressure is 600 ATM.

The resulting tool is not time-stable liposomes that have not passed the test, accelerated aging, and liposomal tool stratified, was not homogeneous.

Example 3. Anti-cellulite liposomal agent.

In water (up to 100 kg) temperature 30C add 6 kg of the extract smoke, 6 m extract of anise, 30 kg of lecithin and mix all to education the Finance homogeneous mass. Next, we take 0.6 kg of the extract of pink pepper, add to it 0,06 kg of antioxidant butylhydroxytoluene, heated with stirring to 45C and continue to stir until complete dissolution of butylhydroxytoluene. Then 1 kg of preservative, Germaben and the mixture butylhydroxytoluene blended with pink pepper added to a mixture of water, lecithin, extracts of smoke and APIs. Next, using high-speed stirrers Ultra Turrax for 10 min with a speed of 1500 Rev/min conducting intensive mixing of the mass. The resulting mixture is expanded through a high-pressure homogenizer. Spend 2 cycle run, the working pressure is 600 ATM.

The resulting tool is a anti-cellulite liposomes are stable in time (passed the test for accelerated aging and change appearance over time), but research on the microscope showed that the result of liposomes having multiple layers (almost complete lack of internal space) and therefore has very little effectiveness of the inclusion in the internal phase water-soluble assets. Thus will not be achieved strengthening of the water-soluble active substances due to transport them to the deeper layers of the skin, thereby lost effective anti-cellulite effect Dunn is th formula.

Comparative clinical studies have been conducted on 18 volunteers-women aged 18 to 50 years. All the women had expressed signs of Celica with a primary lesion of the thigh, the gluteal regions and belly.

Women put the cream on the area of the lesions, followed by rubbing in for 3 minutes 2 times a day, 28 days in a row.

At 0 and day 29 of the study visually and by palpation evaluated the severity of cellulite, flexibility and smartness of the skin, as well as made to measure hip size and waist volunteers. The results are shown in the form of tables and charts 1 and 2.

Name symptomsNumber of subjects (out of 18)who have recorded a marked improvement on the 29th day of research
Reduction of waist15
Reduction of thighs16
The severity of cellulite18
Skin elasticity17
Smartness skin18

1. Anti-cellulite liposomal tool, characterized by the fact that h is about contains enclosed in the liposomes of lecithin water-soluble extract of Cotinus (Buxus sinica) and Anise (Pimpinella anisum) and oil-soluble extract of Pink pepper (Schinus terebinthifolius), when this water-soluble extracts of Smoke tree (Buxus sinica) and Anise (Pimpinella anisum) is enclosed in the internal phase of the liposome, and oil-soluble extract of Pink pepper (Schinus terebinthifolius) is enclosed in the membrane of liposomes.

2. Anti-cellulite liposomal tool according to claim 1, characterized in that the content of lecithin in amounts from 5 to 25 wt.%.

3. Anti-cellulite liposomal tool according to claim 2, characterized in that as the use of lecithin soy lecithin.

4. Anti-cellulite liposomal tool according to claim 1, characterized in that its content of oil-soluble extract of Pink pepper is from 0.1 to 1 wt.%, the content of water-soluble extract of Cotinus is from 1 to 10 wt.%, and the content of water-soluble extract of Anise from 1 to 10 wt.%.



 

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2 cl, 2 tbl, 2 ex

FIELD: medicine, oncology, amino acids.

SUBSTANCE: invention relates, in particular, to the development of an antitumor preparation based on natural substances. Invention relates to an amino acid preparation comprising at least one modified essential amino acid obtained by treatment of amino acid by ultraviolet radiation (UV) at wavelength 250-350 nm for 12-80 h at temperature 15-30oC or with ozone at temperature 15-25oC. The modified amino acid has no toxicity for health cells. Also, invention relates to a method for preparing such preparation. Invention provides the development of an antitumor preparation based on modified amino acids and expanded assortment of antitumor preparations being without cytotoxicity for normal cells.

EFFECT: valuable medicinal antitumor properties of preparation.

8 cl, 4 tbl, 2 dwg, 4 ex

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